Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro.

The roots of Krameria lappacea are used traditionally against oropharyngeal inflammation. So far, the astringent and antimicrobial properties of its proanthocyanidin constituents are considered to account for the anti-inflammatory effect. The aim of the present study was to characterize pharmacologically a lipophilic extract of K. lappacea roots and several isolated lignan derivatives (1-11) in terms of their putative anti-inflammatory activity. The dichloromethane extract (ID50 77 µg/cm²) as well compounds 1-11 (ID50 0.31-0.60 µmol/cm²) exhibited topical antiedematous properties comparable to those of indomethacin (ID50 0.29 µmol/cm²) in a mouse ear in vivo model. Two of the most potent compounds, 2-(2-hydroxy-4-methoxyphenyl)-5-(3-hydroxypropyl)benzofuran (5) and (+)-conocarpan (7), were studied regarding their time-dependent edema development and leukocyte infiltration up to 48 h after croton oil-induced dermatitis induction, and they showed activity profiles similar to that of hydrocortisone. In vitro studies of the isolated lignan derivatives demonstrated the inhibition of NF-κB, cyclooxygenase-1 and -2, 5-lipoxygenase, and microsomal prostaglandin E2 synthase-1 as well as antioxidant properties, as mechanisms possibly contributing to the observed in vivo effects. The present findings not only support the ethnopharmacological use of K. lappacea roots but also reveal that the isolated lignan derivatives contribute strongly to the anti-inflammatory activity of this herbal drug.

In vivo anti-inflammatory and in vitro antioxidant activities of Mediterranean dietary plants.

Five hydroalcoholic extracts of edible plants from Calabria region (Italy) used in local traditional medicine for the treatment of inflammatory diseases were evaluated for their in vivo topical anti-inflammatory activity (inhibition of croton oil-induced ear oedema in mice) and in vitro antioxidant and antiradical properties (inhibition of linoleic acid oxidation and bovine brain liposomes peroxidation, DPPH radical scavenging). All the extracts showed an anti-inflammatory effect: 300 microg/cm(2) provoked oedema reductions ranging from 21 to 27%. All the extracts exerted also radical scavenging and/or antioxidant properties, the most active plant being Mentha aquatica L. (Lamiaceae) which contained the highest amount of phenolics (337 mg/g) and of flavonoids (15.75 mg/g). Moreover, the content and the composition of sterols were assessed by GC-MS in the examined plants Borago officinalis L. (Boraginaceae) contained the highest number of sterols.

Evaluation of the topical anti-inflammatory activity of ginger dry extracts from solutions and plasters.

In this study the skin permeation and the topical anti-inflammatory properties of ginger extracts were investigated. A commercial ginger dry extract (DE) and a gingerols-enriched dry extract (EDE) were evaluated for their in vivo topical anti-inflammatory activity by inhibition of Croton oil-induced ear oedema in mice. Furthermore, the feasibility of an anti-inflammatory plaster containing DE or EDE was evaluated. Since the in vivo activity was evaluated in mice, the ex vivo skin permeation study was performed by using mouse skin or human epidermis. The DE from the acetonic solution exerted a dose-dependent topical anti-inflammatory activity (ID (50) = 142 microg/cm (2)), not far from that of the potent reference substance indomethacin (ID (50) = 93 microg/cm (2)). Similarly, the EDE induced a dose-dependent oedema reduction though its potency (ID (50) = 181 microg/cm (2)) was slightly lower than that of DE. Increase of the 6-gingerol concentration in the extract did not improve the anti-inflammatory activity. The medicated plasters, containing 1 mg/cm (2) of the commercial DE or EDE, had good technological characteristics and exerted a significant antiphlogistic effect, too. By using the plaster containing EDE, the 6-gingerol amount that permeated through human epidermis was 6.9 microg/cm (2) while the amount that passed through mouse skin was 22.1 microg/cm (2). Nevertheless, the amounts of 6-gingerol permeated through human epidermis and mouse skin in the early period (8h) were comparable (p > 0.3). This preliminary result suggests that the anti-inflammatory effect observed in mice could also be exerted in humans.

Topical antiinflammatory activity of an innovative aqueous formulation of actichelated propolis vs two commercial propolis formulations.

A novel aqueous commercial formulation of a new hydrophilic propolis product (Actichelated((R)) Propolis, contained in 'LeniGola PropolEffect Spray Senza Alcohol'; Pharbenia, Milan, Italy) was evaluated for its topical antiinflammatory activity in comparison with a hydroglyceric propolis spray solution ('Propoli LeniGola Spray Senza Alcool'; Pharbenia, Milan, Italy) and a hydroalcohol preparation ('Propoli LeniGola Spray Forte'; Pharbenia, Milan, Italy). Actichelated propolis (Actimex, Trieste, Italy) is a multicomposite material obtained with a patented technology, mechano-chemical activation, which application led to a new hydrosoluble form of propolis. Each propolis preparation provoked a dose-dependent inhibition of the croton oil-induced ear oedema in mice. Considering the administered doses of flavonoids, 'LeniGola PropolEffect Spray Senza Alcool' (ID(50) = 13.6 microL/cm(2), corresponding to 13.6 microg flavonoids/cm(2)) is slightly more active than the hydroglyceric formulation 'Propoli LeniGola Spray' (ID(50) = 13.7 microL/cm(2), corresponding to 20.6 microg flavonoids/cm(2)) and six times more active than the hydroalcohol preparation 'Propoli LeniGola Spray Forte' (ID(50) = 5.5 microL/cm(2), corresponding to 82.5 microg flavonoids/cm(2)). As a reference, 15 microL/cm(2) of the commercial sprays Tantum Verde and Froben, containing 37.5 or 45 microg of the non-steroidal antiinflammatory drugs benzidamine hydrochloride or flurbiprofen, induced 18% and 35% oedema inhibition, respectively.